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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-BPI-460372
BPI-460372

Chemical Structure : BPI-460372

CAS No.: 2762619-63-4

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BPI-460372 (BPI460372)

货号: PC-23994Not For Human Use, Lab Use Only.

BPI-460372 is a potent, orally available, covalent, irreversible inhibitor of TEAD1/3/4, irreversibly binds to the cysteine residue in the TEAD palmitoylation pocket, preventing TEAD palmitoylation and inhibiting its biological function.

规格 价格 库存 数量
5 mg ￥1580 In stock
10 mg ￥2480 In stock
25 mg ￥4280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BPI-460372 is a potent, orally available, covalent, irreversible inhibitor of TEAD1/3/4, irreversibly binds to the cysteine residue in the TEAD palmitoylation pocket, preventing TEAD palmitoylation and inhibiting its biological function.
BPI-460372 significantly inhibits the expression of a TEAD-responsive element reporter, as well as the mRNA of downstream target genes such as CTGF and CYR61 in NF2-deficient cells.
BPI-460372 strongly inhibited the proliferation of tumor cells harboring Hippo pathway aberrations.
BPI-460372 significantly suppressed tumor growth in NF2-deficient or LATS1/2 mutation xenograft models.

物理化学性质&存储条件

分子量 407.33
分子式 C18H13F4N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(1-(2-Fluoroacryloyl)azetidin-3-yl)-3-(4-(trifluoromethyl)phenyl)-1,3-dihydro-2H-imidazo[4,5-b]pyrazin-2-one

参考文献

1. Xiaohong Han, et al. Cancer Res (2024) 84 (6_Supplement): 7575.

2. Hongling Shen, et al. Cancer Res (2023) 83 (7_Supplement): 501.

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